Abstract
The natural flavonoids as human digestive enzymes, such as α-glucosidase, α-amylase and aldose reductases inhibitors, have attracted great interest among researchers. The objective of this review is to overview the structures required of flavonoids for inhibiting these digestive enzymes. The hydroxylation on rings A and B of flavonoids improved the inhibition against these digestive enzymes. The hydroxylation on A-ring of flavones and isoflavones, especially at C-5 and C-7, significantly enhanced the inhibitory activities against digestive enzymes and the hydroxylation on positions C-3′ and C-4′ of B-ring of flavonoids remarkably improved the inhibition. The hydrogenation of the C2=C3 double bond on flavonoids decreased the inhibitory effects. The glycosylation of hyroxyl group on flavonoids weakened the inhibition against α-amylases and α-glucosidases. The glycosylation on 7-OH and 4'-OH of flavonoids significantly decreased the inhibition for aldose reductases. The glycosylation on 3-OH of flavonoids significantly increased or little affected the inhibition on aldose reductases. The methylation and methoxylation of flavonoids obviously weakened the inhibitory effects against α-amylase. The methylation and methoxylation of the hydroxyl group at C-3, C-3' and C-4' of flavonoids decreased or little affected the inhibitory potency against aldose reductases. And, the methylation and methoxylation of the hydroxyl groups at 5, 6, and 8 significantly increased the inhibitory capacity for aldose reductases. The methylation and methoxylation of flavonoids obviously affected the inhibitory effect for α-glucosidase in vitro depending on the replaced site.
Keywords: Flavonoids, α-glucosidase, α-amylase, Aldose reductase, Structure-activity relationship, isoflavones, apigenin, Soybean, D-sorbitol, α-amylases
Anti-Cancer Agents in Medicinal Chemistry
Title:Structures Required of Flavonoids for Inhibiting Digestive Enzymes
Volume: 12 Issue: 8
Author(s): Hui Cao and Xiaoqing Chen
Affiliation:
Keywords: Flavonoids, α-glucosidase, α-amylase, Aldose reductase, Structure-activity relationship, isoflavones, apigenin, Soybean, D-sorbitol, α-amylases
Abstract: The natural flavonoids as human digestive enzymes, such as α-glucosidase, α-amylase and aldose reductases inhibitors, have attracted great interest among researchers. The objective of this review is to overview the structures required of flavonoids for inhibiting these digestive enzymes. The hydroxylation on rings A and B of flavonoids improved the inhibition against these digestive enzymes. The hydroxylation on A-ring of flavones and isoflavones, especially at C-5 and C-7, significantly enhanced the inhibitory activities against digestive enzymes and the hydroxylation on positions C-3′ and C-4′ of B-ring of flavonoids remarkably improved the inhibition. The hydrogenation of the C2=C3 double bond on flavonoids decreased the inhibitory effects. The glycosylation of hyroxyl group on flavonoids weakened the inhibition against α-amylases and α-glucosidases. The glycosylation on 7-OH and 4'-OH of flavonoids significantly decreased the inhibition for aldose reductases. The glycosylation on 3-OH of flavonoids significantly increased or little affected the inhibition on aldose reductases. The methylation and methoxylation of flavonoids obviously weakened the inhibitory effects against α-amylase. The methylation and methoxylation of the hydroxyl group at C-3, C-3' and C-4' of flavonoids decreased or little affected the inhibitory potency against aldose reductases. And, the methylation and methoxylation of the hydroxyl groups at 5, 6, and 8 significantly increased the inhibitory capacity for aldose reductases. The methylation and methoxylation of flavonoids obviously affected the inhibitory effect for α-glucosidase in vitro depending on the replaced site.
Export Options
About this article
Cite this article as:
Cao Hui and Chen Xiaoqing, Structures Required of Flavonoids for Inhibiting Digestive Enzymes, Anti-Cancer Agents in Medicinal Chemistry 2012; 12 (8) . https://dx.doi.org/10.2174/187152012802650110
DOI https://dx.doi.org/10.2174/187152012802650110 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Current Metabolomic Methodologies & their Application to Thermal Stress
Current Metabolomics Targeting Leukostasis for the Treatment of Early Diabetic Retinopathy
Cardiovascular & Hematological Disorders-Drug Targets Neurological Aspects of Medical Use of Cannabidiol
CNS & Neurological Disorders - Drug Targets Seaweed Polysaccharides - New Therapeutic Insights Against the Inflammatory Response in Diabetic Nephropathy
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry The Potential Role of Angiotensin Converting Enzyme and Vasopeptidase Inhibitors in the Treatment of Diabetic Neuropathy
Current Drug Targets Periodontal Disease and Potential Association with Systemic Diseases and Conditions (Mini-review)
Applied Clinical Research, Clinical Trials and Regulatory Affairs Advanced Glycation: Implications in Tissue Damage and Disease
Protein & Peptide Letters Prevention and Treatment for Chemotherapy-Induced Peripheral Neuropathy: Therapies Based on CIPN Mechanisms
Current Neuropharmacology Role of Advanced Glycation End Products (AGEs) in Osteoporosis in Diabetes
Current Drug Targets Anaemia in Diabetes: An Emerging Complication of Microvascular Disease
Current Diabetes Reviews Childhood Maltreatment and Stress-Related Psychopathology: The Epigenetic Memory Hypothesis
Current Pharmaceutical Design Unfolded Protein Response in Chronic Obstructive Pulmonary Disease: Smoking, Aging and Disease: A SAD Trifecta
Current Molecular Medicine Patent Selections:
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Novel Strategies for Preventing Diabetes and Obesity Complications with Natural Polyphenols
Current Medicinal Chemistry Glia as a Turning Point in the Therapeutic Strategy of Parkinsons Disease
CNS & Neurological Disorders - Drug Targets Patients Stratification Strategies to Optimize the Effectiveness of Scavenging Biogenic Aldehydes: Towards a Neuroprotective Approach for Parkinson's Disease
Current Neuropharmacology Prolylcarboxypeptidase Gene Expression in the Heart and Kidney: Effects of Obesity and Diabetes
Cardiovascular & Hematological Agents in Medicinal Chemistry Signaling Pathways Involved in Physiopathology of Pancreatic β -Cells
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Pathogenic Mechanisms and Therapeutic Strategies in Spinobulbar Muscular Atrophy
CNS & Neurological Disorders - Drug Targets Is β-catenin neutralization cross-involved in the mechanisms mediated by natalizumab action?
Current Molecular Medicine